Design, Synthesis and Antimycobacterial Activity of Novel Imidazo[1,2-a]pyridine Amide-Cinnamamide Hybrids
We report herein the design and synthesis of a series of novel imidazo[1,2-a]pyridine amide-cinnamamide hybrids linked via an alkyl carbon chain. All 38 new hybrids were evaluated for their antimycobacterial activity against M. tuberculosis (MTB) H37Rv ATCC 27294 using the microplate Alamar Blue ass...
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MDPI AG
2015-12-01
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Series: | Molecules |
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Online Access: | http://www.mdpi.com/1420-3049/21/1/49 |
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author | Linhu Li Zhuorong Li Mingliang Liu Weiyi Shen Bin Wang Huiyuan Guo Yu Lu |
author_facet | Linhu Li Zhuorong Li Mingliang Liu Weiyi Shen Bin Wang Huiyuan Guo Yu Lu |
author_sort | Linhu Li |
collection | DOAJ |
description | We report herein the design and synthesis of a series of novel imidazo[1,2-a]pyridine amide-cinnamamide hybrids linked via an alkyl carbon chain. All 38 new hybrids were evaluated for their antimycobacterial activity against M. tuberculosis (MTB) H37Rv ATCC 27294 using the microplate Alamar Blue assay (MABA). Although the hybrids are less active than the two reference compounds, the promising activity (MICs: 4 μg/mL) of 2,6-dimethylimidazo[1,2-a]pyridine amide-cinnamamide hybrids 11e and 11k could be a good starting point to further find new lead compounds against multi-drug-resistant tuberculosis. |
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id | doaj.art-74c2c1bcb0da4860b15eca8c9d7c3fe8 |
institution | Directory Open Access Journal |
issn | 1420-3049 |
language | English |
last_indexed | 2024-12-13T16:26:00Z |
publishDate | 2015-12-01 |
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series | Molecules |
spelling | doaj.art-74c2c1bcb0da4860b15eca8c9d7c3fe82022-12-21T23:38:36ZengMDPI AGMolecules1420-30492015-12-012114910.3390/molecules21010049molecules21010049Design, Synthesis and Antimycobacterial Activity of Novel Imidazo[1,2-a]pyridine Amide-Cinnamamide HybridsLinhu Li0Zhuorong Li1Mingliang Liu2Weiyi Shen3Bin Wang4Huiyuan Guo5Yu Lu6Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, ChinaInstitute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, ChinaInstitute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, ChinaZhejiang Starry Pharmaceutical Co. Ltd., Xianju 317300, ChinaBeijing Key Laboratory of Drug Resistance Tuberculosis Research, Department of Pharmacology, Beijing Tuberculosis and Thoracic Tumor Research Institute, Beijing Chest Hospital, Capital Medical University, Beijing 101149, ChinaInstitute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, ChinaBeijing Key Laboratory of Drug Resistance Tuberculosis Research, Department of Pharmacology, Beijing Tuberculosis and Thoracic Tumor Research Institute, Beijing Chest Hospital, Capital Medical University, Beijing 101149, ChinaWe report herein the design and synthesis of a series of novel imidazo[1,2-a]pyridine amide-cinnamamide hybrids linked via an alkyl carbon chain. All 38 new hybrids were evaluated for their antimycobacterial activity against M. tuberculosis (MTB) H37Rv ATCC 27294 using the microplate Alamar Blue assay (MABA). Although the hybrids are less active than the two reference compounds, the promising activity (MICs: 4 μg/mL) of 2,6-dimethylimidazo[1,2-a]pyridine amide-cinnamamide hybrids 11e and 11k could be a good starting point to further find new lead compounds against multi-drug-resistant tuberculosis.http://www.mdpi.com/1420-3049/21/1/49imidazo[1,2-a]pyridine amide-cinnamamide hybridsdesignsynthesisantimycobacterial activity |
spellingShingle | Linhu Li Zhuorong Li Mingliang Liu Weiyi Shen Bin Wang Huiyuan Guo Yu Lu Design, Synthesis and Antimycobacterial Activity of Novel Imidazo[1,2-a]pyridine Amide-Cinnamamide Hybrids Molecules imidazo[1,2-a]pyridine amide-cinnamamide hybrids design synthesis antimycobacterial activity |
title | Design, Synthesis and Antimycobacterial Activity of Novel Imidazo[1,2-a]pyridine Amide-Cinnamamide Hybrids |
title_full | Design, Synthesis and Antimycobacterial Activity of Novel Imidazo[1,2-a]pyridine Amide-Cinnamamide Hybrids |
title_fullStr | Design, Synthesis and Antimycobacterial Activity of Novel Imidazo[1,2-a]pyridine Amide-Cinnamamide Hybrids |
title_full_unstemmed | Design, Synthesis and Antimycobacterial Activity of Novel Imidazo[1,2-a]pyridine Amide-Cinnamamide Hybrids |
title_short | Design, Synthesis and Antimycobacterial Activity of Novel Imidazo[1,2-a]pyridine Amide-Cinnamamide Hybrids |
title_sort | design synthesis and antimycobacterial activity of novel imidazo 1 2 a pyridine amide cinnamamide hybrids |
topic | imidazo[1,2-a]pyridine amide-cinnamamide hybrids design synthesis antimycobacterial activity |
url | http://www.mdpi.com/1420-3049/21/1/49 |
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